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Neuro Pharm Flashcards

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1
Q

Glaucoma drugs: classes and specific drugs

A
  1. alpha agonists: epinephrine, brimonidine
  2. beta blockers: timolol, betaxolol, careolol
  3. diuretics: acetazolamide
  4. cholinomimetics:
    direct: carbachol, pilocarpine
    indirect: physostigmine, echothiophate
  5. prostaglandin: latanoprost
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2
Q

Glaucoma - Epinephrine

  1. mechanism
  2. side effects
  3. c/i
A
  1. alpha agonist: decrease aq humour synthesis through vasoconstriction
  2. mydriasis, stinging
  3. DO NOT USE in closed angle glaucoma
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3
Q

Glaucoma - Brimonidine

  1. mechanism
  2. side effects
A
  1. alpha 2-agonist, decreases aq humor synthesis

2. none

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4
Q

Glaucoma - Beta blockers

  1. mechanism
  2. side effects
A
  1. decrease aq humour secretion
  2. none

timilol, betaxolol, carteolol

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5
Q

Glaucoma - Acetazolamide

  1. mechanism
  2. side effects
A
  1. decrease aq humour secretion by decreasing HCO3- via inhibition of carbonic anhydrase
  2. none
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6
Q

Glaucoma - Cholinomimetics

  1. mechanism
  2. side effects
A
  1. Increase outflow of aq humour, contract ciliary muscle (which produces aq humour) and opens trabecular network into canal of Schlemm
  2. miosis, cyclospasm (accomodate)
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7
Q

Which glaucoma drug do you use in an emergency?

A

Pilocarpine

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8
Q

Glaucoma - Latanoprost

  1. mechanism
  2. side effects
A
  1. Prostaglandin (PGFa2), increase outflow of aq humour

2. Darkens iris (browning)

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9
Q

Opioid analgesics - drugs

A 
Morphine
Fentanyl
Codeine
Heroin
Methadone
Meperidine
Dextromethorphan
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10
Q

Opioid analgesics - mechanism

A

Agonist at opioid receptors, mu (morphine), delta (enkephalin), kappa (dynorphin)

Open K close Ca channels –> decrease synaptic transmission

Inhibit release of ACh, NE, 5HT, glutamate, substance P

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11
Q

Opioid analgesics - use

A 
Pain
Cough suppression (dextromethorphan)
Diarrhea (loperamide and diphenoxylate)
Acute pulmonary edema
Maintenance program for addicts (methadone)
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12
Q

Which opioid is used for cough suppression?

A

Dextromethorphan

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13
Q

Which opioids are used for diarrhea?

A

Loperamide and diphenoxylate

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14
Q

Which opioids are used for maintenance in drug addicts?

A

Methadone

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15
Q

Toxicity of opioid analgesics

A 
Tolerance
Respiratory depression
Constipation
Miosis
CNS depression with other drugs
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16
Q

What do you treat opioid toxicity with?

A

Opioid receptor antagonists:
naltrexone
naloxone

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17
Q

What do you NOT develop tolerance to when using opioids?

A

Miosis

Constipation

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18
Q

Butorphanol

Mechanism
Use
Toxicity

A
  1. Partial agonist at opioid mu receptors, agonist at kappa
  2. Pain, causes less respiratory depression than full agonists
  3. Causes withdrawal if on full agonists
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19
Q

Which opioid causes less respiratory depression in comparison to other opioids?

A

Butorphanol

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20
Q

Tramadol

  1. Mechanism
  2. Use
  3. Toxicity
A
  1. Weak opioid agonist, inhibits Serotonin and NE reuptake (works on multiple neurotransmitters)
  2. chronic pain
  3. decreases seizure threshold
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21
Q

Phenytoin

  1. Tx’s which seizures
  2. Mechanism
  3. Which drug can be used parenterally?
A
  1. Simple Partial
    Simple Complex
    1st line for Generalized Tonic-Clonic
    1st line for Status
  2. Use dependent blockade of Na+ channels, decrease refractory period, inhibit glutamate release form excitatory presynaptic neurons
  3. Fosphenytoin
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22
Q

Phenytoin toxicity

A 
Gingival hyperplasia in kids
Hirsutism
Megaloblastic anemia (decreases folate absorption)
Teratogenesis (fetal hydantoin syndrome)
SLE-like syndrome
Cyt-P450 inducer
SJS
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23
Q

Carbamezapine

  1. Tx’s which seizures
  2. Mechanism
  3. SE
A

1st line for all Simple Partial, Simple Complex, Generalized Tonic-Clonic

  1. Increases Na channel inactivation
  2. diplopia, ataxia, blood dyscrasias, liver tox, teratogenesis, cP450 inducer, SIADH, SJS
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24
Q

Which drug is 1st line for trigeminal neuralgia?

A

Carbamezapine

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25
Lamotrigine 1. Tx's which seizures 2. Mechanism 3. SE
1. PS, PC, GTC 2. Blocks voltage-gated Na channels 3. SJS
26
Gabapentin 1. Tx's which seizures 2. Mechanism 3. SE 4. other uses
1. PS, PC, GTC 2. GABA analogue, blocks high voltage activated Ca channels 3. Sedation, ataxia 4. peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder
27
Topiramate 1. Tx's which seizures 2. Mechanism 3. SE 4. other uses
1. PS, PC, GTC 2. Blocks Na channels, increases GABA action 3. sedation, metal dulling, kidney stones, weight loss 4. migraine preention
28
Phenobarbital 1. Tx's which seizures 2. Mechanism 3. SE
1. PS, PC, GTC 2. Increases duration of Cl- channel opening, increases GABA action 3. sedation, tolerance, dependence, cP450 inducer
29
Which AED is the first line for kids and pregnant women?
Phenobarbital
30
Which drugs are first line for GTC seizures?
Phenytoin Carbamezapine Valproic acid
31
Valproic acid 1. Tx's which seizures 2. Mechanism 3. SE 4. other uses
1. PS, PC, 1st line for GTC 2. Increase Na inactivation, increase GABA action via GABA transaminase inhibition 3. GI distress, hepatotoxicity, neural tube defects, tremor, weight gain 4. myoclonic seizures, bipolar disorder
32
Which AED is also used for myoclonic seizures?
Valproic acid
33
Ethosuximide 1. Tx's which seizures 2. Mechanism 3. SE
1. 1st line for absence seizures 2. Block Ca channels in thalamus 3. fatigue, GI distress, headact, itching, SJS, urticaria
34
Benzo's 1. Tx's which seizures 2. Mechanism
1. first line for acute status epilepticus | 2. increase frequency of Cl- channel opening
35
Tiagabine 1. Tx's which seizures 2. Mechanism
1. PS, PC | 2. inhibit GABA reuptake
36
Vigabatrin 1. Tx's which seizures 2. Mechanism
1. PS, PC | 2. inhibits GABA transaminase, increasing GABA
37
Levetiracetam 1. Tx's which seizures 2. Mechanism
1. PS, PC, GTC | 2. Unknown
38
Which AEDs are first line for status epilepticus?
Prophylaxis: Phenytoin Acute: Benzo
39
Which AED is used for seizures in eclampsia?
Benzo MgSO4 is first line
40
What are the only drugs for absence seizures?
ethosuximide is first line for absence and is only used for that valproic acid can be used
41
Most of the seizure drugs are associated with what classes?
simple, complex, tonic-clonic
42
Benzodiazepine toxicities
Sedation Tolerance Dependance
43
Stevens-Johnsons syndrome Sx's AEDs that have this SE
1. Prodrome of malaise and fever Rapid onset erythematous/purpuric macules (oral, ocular, genital) Epidermal necrosis and sloughing 2. Ethosuximide Carbamezapine Lamotrigine Phenytoin
44
Phenytoin is also what type of drug in addition to being an AED?
Class I antiarrhythmic
45
Barbiturates: 1. Examples of drugs 2. Use 3. Toxicites 4. Tx overdose?
1. Phenobarbital, pentobarbital, Thiopental , secobarbital 2. Anxiety, seizures, insomnia, induction for anesthesia 3. additive CNS depression respiratory/CV depression induction of Cyt-P450 4. symptom management -- assist respiration and increase BP
46
Which AED is contraindicated in porphyria?
Barbiturates
47
Benzodiazepines 1. use 2. list short-acting drugs 3. toxicity
1. anxiety, spasticity, epilepticus, detox from EtOH, night terrors, sleep walking, general anesthetic, hypnotic 2. Triazolam Oxazepam Midazolam 3. dependance additive CNS depression with EtOH less risk of respiratory depression and coma
48
How do you Tx benzo overdose?
Flumazenil GABA receptor antagonist
49
Which benzo's have the highest addictive potential?
Short acting Triazolam Oxazepam Midazolam
50
Which 2 AEDs are used for acute status epileptices?
Diazepam Lorazepam (Benzo's)
51
How do CNS drugs cross BBB?
1. soluble in lipid OR 2. transporter
52
Drugs with decreased solubility in the blood have:
rapid induction and recovery times
53
Drugs with increased solubility in lipids have:
Increased potency
54
Potency of anesthetic drug =
1/MAC MAC = minimal alveolar concentration
55
What does a large MAC mean in terms of potency?
low potency
56
MAC
minimal alveolar concentration at which 50% of population is anesthetized
57
how do barbiturates and benzos effect the GABA receptor?
barbiturates increase the duration of the Cl- channel opening while benzos increase the frequency
58
1. What are the nonbenzodiazepine hypnotics? 2. MOA 3. clinical use 4. toxicity
1. zolpidem, zaleplon, eszopliclone 2. BZ1 subtype of GABAR, reversed with flumazenil 3. insomnia 4. ataxia, heaches, confusion
59
Halothane has increased blood and lipid solubility, what does this mean in terms of potency and induction?
increased blood solubility: slow induction increased lipid solubility: high potency
60
Mechanism of anesthetic action in lungs
increases rate and depth of ventilation
61
Mechanism of anesthetic action in blood
increased blood solubility: increase gas required to saturate blood --> slow induction time
62
Mechanism of anesthetic action in tissue (i.e. brain)
increased solubility: increased gas required to saturate tissue --> slower onset of action
63
Inhaled anesthetics 1. Drug examples 2. Mechanism 3. Effects 4. Toxicity
1. Halothane, isoflurane, nitrous oxide 2. unknown 3. myocardial and respiratory depression nausea/emesis increased cerebral blood flow (decreased cerebral metabolic demand) 4. Hepatotoxicity - halothane Nephrotoxicity - methoxyflurane Proconvulsant - enflurane Malignant hyperthermia
64
How do you treat malignant hyperthermia?
dantrolene
65
IV anesthetics (5)
``` Barbiturates Benzodiazepine Ketamine Opiates Propofol ```
66
Thiopental 1. Potency, lipid solubility, entry time into brain 2. use 3. effect terminated by 4. effect on cerebral blood flow
IV anesthetic, barbiturate 1. high potency, high lipid solubility, rapid entry 2. induction anesthesia, short surgical procedures 3. redistribution into fat and tissues 4. decreases cerebral blood flow
67
Benzo's 1. use in anesthesia 2. used in conjuction with 3. toxicity
1. IV anesthetic, midazolam most commonly used for endoscopy 2. gas anesthetics and narcotics 3. severe post-op respiratory depression, amnesia
68
Ketamine (arylcyclohexamine) 1. analog of 2. blocks which receptors 3. simulates 4. side effects
1. PCP, dissociative anesthesia 2. NMDA 3. CV system 4. disorientation, hallucination, bad dreams, increases cerebral blood flow
69
Opiates used as IV anesthetics
Morphine, fentanyl
70
Propofol 1. use 2. mechanism
1. IV rapid induction of anesthesia, short procedures 2. potentiates GABA -A Less post-op nausea than thiopental
71
Ester local anesthetics
Procaine, cocaine, tetracaine
72
Amide local anesthetics
lidocaine, mepivacaine, bupivacaine | amides have 2 i's each
73
Local anesthetics: mechanism
block Na channels binds better to activated Na channels, so most effective in rapidly firing neurons
74
Tertiary local amides penetrate membrane in what form and bind to ion channels in what form?
penetrate in uncharged | bind in charged form
75
In infected (acidic) tissue, how must local anesthetics be administered differently?
Alkaline anesthetics are charged and can't penetrate acidic membrane effectively, so must administer more
76
Order of nerve blockade in local anesthetics
small fibers > large fibers myelinated fibers > unmyelinated Size factor predominates over myelination.
77
Order of sensory loss in local anesthetics
Pain>temperature>touch>pressure
78
Local anesthetics are usually given with what drug and why?
Vasoconstrictors (epi), they enhance local action *except cocaine
79
Local anesthesia toxicity
``` CNS excitation Severe CV toxicity (bupivacaine) HTN Hypotension Arrhythmias (cocaine) ```
80
NMJ blockers 1. use 2. selective for which receptor 3. types
1. muscle paralysis in surgery or mechanical ventilation 3. Motor nicotinic 3. Depol and Non-depol
81
Succinylcholine 1. class 2. reversal of blockade 3. complications
1. cholinomimetic, NMJ depolarizing blocker 2. Phase 1: prolonged depol, no antidote , potentiated by cholinesterase inhibitors Phase 2: repolarized but blocked, can reverse with AChE inhibitors (neostigmine) 3. Hypercalemia, Hyperkalemia, malignant hyperthermia
82
Non-depolarizing NMJ blockers 1. examples 2. mechanism 3. reversal of blockade
1. tubocurarine, atracurium, pancuronium, etc. 2. competitive antagonists for ACh 3. AChE inhibitors (neostigime, edrophonium, etc.)
83
Dantrolene: use and mechanism
tx for malignant hyperthermia and neuroleptic malignant syndrome prevents release of Ca from sarcoplasmic reticulum of skeletal muscle
84
Malignant hyperthermia is caused by
concomitant use of inhalational anesthetics (except N2O) and succinylcholine
85
Parkinson's has excess____ activity
cholinergic due to loss of dopaminergic neurons
86
PD drug classes
1. dopamine agonists - Bromocriptine 2. drugs that increase dopamine - Amantadine, L-dopa/carbidopa 3. prevent dopamine breakdown - Selegiline 4. decrease cholinergic activity - Benztropine
87
Dopamine agonists in PD: examples side effects
1. Bromocriptine (ergot), pramipexole, ropinorole (non-ergot, preferred) 2. gambling
88
Amantadine in PD
Increases dopamine release also used as antiviral against influenza A toxicity: ataxia
89
Selegiline 1. MOA 2. examples 3. adjunctive to what PD drug 4. toxicity
1. selective MAO-B inhibitor, which prefers metabolism of dopamine instead of NE or 5-HT 2. Entacapone, tocapone (COMT inhibitors) 3. L-dopa 4. enhance adverse effects of L-dopa
90
Benztropine in PD: MOA
anti-muscarinic (decreased cholinergic activity), improves tremor and rigidity, but little effect on bradykinesia Park your Benz""
91
L-Dopa/carbidopa toxicity
arrhythmias from peripheral conversion of L-dopa Long-term: dyskinesia after administration Short-term: akinesia b/w doeses
92
Why is carbidopa given in PD?
peripheral decarboxylase inhibitor decreases peripheral side effects of L-dopa and increases bioavailability in brain
93
AD Drugs (2) 1. MOA 2. toxicity
Memantine 1. NMDA receptor antagonist, helps prevent excitotoxicity mediated by Ca 2. dizziness, confusion, hallucinations Donezapil, galantamine, rivastigmine 1. AChE inihibitor 2. Nausea, dizziness insomnia
94
Huntington's Drugs 1. alterations in NTs 2. drug classes and examples
1. Increased dopamine, decreased GABA and ACh 2. Reserpine + tetrabenzine - amine depleting Haloperidol - dopamine receptor antagonist
95
Sumatriptan 1. MOA 2. Half-life 3. Use 4. Toxicity 5. c/i in
1. 5-HT agonist. Causes vasoconstriction, inhibits trigeminal activation and vasoactive peptide release. 2. s angina

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